Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma

被引：19

作者：

Fournier, Jean-Francois ^{[1
]}

Bhurruth-Alcor, Yushma ^{[1
]}

Musicki, Branislav ^{[1
]}

Aubert, Jerome ^{[1
]}

Aurelly, Michele ^{[1
]}

Bouix-Peter, Claire ^{[1
]}

Bouquet, Karinne ^{[1
]}

Chantalat, Laurent ^{[1
]}

Delorme, Marion ^{[1
]}

Drean, Benedicte ^{[1
]}

Duvert, Gwenaelle ^{[1
]}

Fleury-Bregeot, Nicolas ^{[2
]}

Gauthier, Blanche ^{[1
]}

Grisendi, Karine ^{[1
]}

Harris, Craig S. ^{[1
]}

Hennequin, Laurent F. ^{[1
]}

Isabet, Tatiana ^{[3
]}

Joly, Florence ^{[1
]}

Lafitte, Guillaume ^{[1
]}

Millois, Corinne ^{[1
]}

Morgentin, Remy ^{[2
]}

Pascau, Jonathan ^{[1
]}

Piwnica, David ^{[1
]}

Rival, Yves ^{[1
]}

Soulet, Catherine ^{[1
]}

Thoreau, Etienne ^{[1
]}

Tomas, Loic ^{[1
]}

机构：

[1] Nestle Skin Hlth R&D, 2400 Route Colles,BP 87, F-06902 Sophia Antipolis, France

[2] Edelris, 115 Ave Lacassagne, F-69003 Lyon, France

[3] Synchrotron Soleil, St Aubin BP 48, F-91192 Gif Sur Yvette, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2018年 / 28卷 / 17期

关键词：

HDAC inhibitors; Squaramide; CTCL; Topical; Mycosis fungoides; DESIGN; CANCER;

D O I：

10.1016/j.bmcl.2018.06.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility and metabolic profiles were shown to be class I, IIB and IV selective.

引用

页码：2985 / 2992

页数：8

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